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Currently, there is no known cure for diabetes. Different pharmaceutical therapies have been approved for the management of type 2 diabetes mellitus (T2DM), some are in clinical trials and they have been classified according to their route or mechanism of action. Insulin types, sulfonylureas, biguanides, alpha-glucosidase inhibitors, thiazolidinediones, meglitinides, sodium–glucose cotransporter type 2 inhibitors, and incretin-dependent therapies (glucagon-like peptide-1 receptor agonists: GLP-1R, and dipeptidyl peptidase 4 inhibitors: DPP-4). Although some of the currently available drugs are effective in the management of T2DM, the side effects resulting from prolonged use of these drugs remain a serious challenge. GLP-1R agonists are currently the preferred medications to include when oral metformin alone is insufficient to manage T2DM. Medicinal plants now play prominent roles in the management of various diseases globally because they are readily available and affordable as well as having limited and transient side effects. Recently, studies have reported the ability of phytochemicals to activate glucagon-like peptide-1 receptor (GLP-1R), acting as an agonist just like the GLP-1R agonist with beneficial effects in the management of T2DM. Consequently, we propose that careful exploration of phytochemicals for the development of novel therapeutic candidates as GLP-1R agonists will be a welcome breakthrough in the management of T2DM and the co-morbidities associated with T2DM. [ABSTRACT FROM AUTHOR]

Background: Recent reports have highlighted the significance of plant bioactive components in drug development targeting neurodegenerative disorders such as Alzheimer's disease (AD). Thus, the current study assessed antioxidant activity and enzyme inhibitory activity of the aqueous extract of Talinum triangulare leave (AETt) as well as molecular docking/simulation of the identified phytonutrients against human cholinesterase activities. Methods: In vitro assays were carried out to assess the 2,2- azinobis (3-ethyl-benzothiazoline-6-sulfonic acid) (ABTS) cation radicals and cholinesterase inhibitory activities of AETt using standard protocols. High performance liquid chromatography coupled with diode-array detection (HPLC–DAD) was employed to identify compounds in AETt. Also, for computational analysis, identified bioactive compounds from AETt were docked using Schrodinger's GLIDE against human cholinesterase obtained from the protein data bank (https://www.rcsb.org/). Results: The results revealed that AETt exhibited a significant concentration-dependent inhibition against ABTS cation radicals (IC50 = 308.26 ± 4.36 µg/ml) with butylated hydroxytoluene (BHT) as the reference. Similarly, AETt demonstrated a significant inhibition against acetylcholinesterase (AChE, IC50 = 326.49 ± 2.01 µg/ml) and butyrylcholinesterase (BChE, IC50 = 219.86 ± 4.13 µg/ml) activities with galanthamine as the control. Molecular docking and simulation analyses revealed rutin and quercetin as potential hits from AETt, having showed strong binding energies for both the AChE and BChE. In addition, these findings were substantiated by analyses, including radius of gyration, root mean square fluctuation, root mean square deviation, as well as mode similarity and principal component analyses. Conclusion: Overall, this study offers valuable insights into the interactions and dynamics of protein–ligand complexes, offering a basis for further drug development targeting these proteins in AD. [ABSTRACT FROM AUTHOR]

Heliotropium indicum are used in ethnomedicine for treating skin rashes, inflammation, tumors and various diseases of microbial origin. Previous work focused on phytochemical constituents, antibacterial activities and isolated compounds. The whole plant was air dried and pulverized (600 g). It was extracted with ethanol and concentrated to dryness in vacuo (20 g). Screening for phytochemical groups was performed using qualitative methods. The antibacterial activity was performed using agar diffusion and antifungal activity using ditch plate method. Compounds were characterized using Gas-chromatography Mass Spectrometry. The results of the phytochemical screening revealed the presence of phenols, saponins, terpenoids and cardiac glycosides. The results further showed the crude extract of the plant to be moderate to strong antibacterial activity with zones of inhibition ranging from 12.0 + 1.6 mm and 25 +1.7 mm. the crude extracts of Heliotropium indicum demonstrated antibacterial properties which confirmed the traditional use of this plant in treating skin rashes and boil. In addition, the presence of Palmitate and Linoleic acid I the plant as revealed in this study justified the use of this plant in treating hypertension. [ABSTRACT FROM AUTHOR]